Chemical Structure : T. cruzi bc1 inhibitor compound 4
CAS No.:
T. cruzi bc1 inhibitor compound 4
Catalog No.: PC-21591Not For Human Use, Lab Use Only.
T. cruzi bc1 inhibitor compound 4 is a highly selective and efficacious T. cruzi cytochrome b inhibitor with IC50 of 6 nM, exhibits potent activity against intracellular amastigotes with EC50 of 0.08 uM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
T. cruzi bc1 inhibitor compound 4 is a highly selective and efficacious T. cruzi cytochrome b inhibitor with IC50 of 6 nM, exhibits potent activity against intracellular amastigotes with EC50 of 0.08 uM.
T. cruzi bc1 inhibitor compound 4 displays no apparent cytotoxicity against either Vero host cells or uninfected HepG2 cells (pEC50 < 4.5).
T. cruzi bc1 inhibitor compound 4 does not inhibit human complex III, does not reduces the calcium loading capacity (CLC) of isolated rat liver mitochondria at 200 uM.
T. cruzi bc1 inhibitor compound 4 (50, 30, or 10 mg/kg bid) exhibits full efficacy against experimental chronic Chagas disease when dosed orally for 5 days in combination with benznidazole (BNZ).
T. cruzi bc1 inhibitor 4 inhibits the Qi active site of T. cruzi cytochrome b, part of the cytochrome bc1 complex of the electron transport chain.
Physicochemical Properties
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M.Wt
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298.35
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Formula
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C16H18N4O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-(2,4-Dimethoxyphenyl)-4,6-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
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References
1. Silvia González, et al. Sci Transl Med. 2023 Dec 13;15(726):eadg8105.
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